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葫芦素D

葫芦素D用途

Cucurbitacin D 是南瓜中的活性成分,可破坏 Hsp90 与两种辅助分子伴侣 Cdc37 和 p23 的相互结合,阻止 Hsp90 客户蛋白 (Her2,Raf,Cdk6,pAkt) 成熟但不诱导热休克反应。具有抗癌作用。

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葫芦素D名称

[ CAS 号 ]:
3877-86-9

[ 中文名 ]:
葫芦素 D

[ 英文名 ]:
Cucurbitacin D

[中文别名 ]:

[英文别名 ]:

Elatericine A
Elatericin A
Cucurbitacin D

葫芦素D生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 代谢酶/蛋白酶 >> HSP

信号通路 >> 细胞周期/DNA损伤 >> HSP

[ 靶点 ]

HSP90

[参考文献]

[1]. Hall JA, et al. Cucurbitacin D Is a Disruptor of the HSP90 Chaperone Machinery. J Nat Prod. 2015 Apr 24;78(4):873-9.

葫芦素D物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
684.0±55.0 °C at 760 mmHg

[ 熔点 ]:
151-152ºC

[ 分子式 ]:
C₃₀H₄₄O₇

[ 分子量 ]:
516.666

[ 闪点 ]:
381.4±28.0 °C

[ 精确质量 ]:
516.308716

[ PSA ]:
132.13000

[ LogP ]:
1.48

[ 蒸汽压 ]:
0.0±4.8 mmHg at 25°C

[ 折射率 ]:
1.582

[ 储存条件 ]:
库房低温,通风,干燥,与食品原料分开存放

葫芦素D毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RC6170000

CHEMICAL NAME :: 19-Nor-9-beta,10-alpha-lanosta-5,23-diene-3,11,22-tri one, 9-methyl-2-beta,16-alpha,20,25- tetrahydroxy-

CAS REGISTRY NUMBER :: 3877-86-9

LAST UPDATED :: 199712

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C30-H44-O7

MOLECULAR WEIGHT :: 516.74

WISWESSER LINE NOTATION :: L E5 B666 CV OV LUTJ B1 E1 FXQ1&V1U1XQ1&1 GQ I1 N1 N1 PQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 8200 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory stimulation Gastrointestinal - hypermotility, diarrhea

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 130,315,1961

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1300 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory stimulation Gastrointestinal - hypermotility, diarrhea

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 130,315,1961

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3400 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory stimulation Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 130,315,1961

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 5 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - other changes Nutritional and Gross Metabolic - body temperature increase

REFERENCE :: CHTPBA Chimica Therapeutica. (Paris, France) V.1-8, 1965-73. For publisher information, see EJMCA5. Volume(issue)/page/year: 4,459,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1750 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory stimulation Gastrointestinal - hypermotility, diarrhea

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 130,315,1961

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4600 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory stimulation Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 130,315,1961

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 960 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory stimulation Gastrointestinal - hypermotility, diarrhea

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 130,315,1961

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 1000 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Gastrointestinal - nausea or vomiting

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 130,315,1961

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 900 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Gastrointestinal - nausea or vomiting

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 130,315,1961

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葫芦素D安全信息

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 海关编码 ]:
29144000